31526-71-3Relevant articles and documents
PROCESSES FOR THE PREPARATION OF APREMILAST AND INTERMEDIATES THEREOF
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Paragraph 0078, (2017/07/29)
Disclosed are processes for the preparation of Apremilast and intermediates for its preparation.
Preparation method of Apremilast and intermediate
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Paragraph 0044; 0045; 0046; 0047, (2016/10/07)
The invention provides a preparation method of Apremilast and its intermediate. The invention provides an Apremilast intermediate as shown in the formula III. According to the preparation method, the compound as shown in the formula III reacts with methanesulfinate to obtain a compound as shown in the formula IV; the compound as shown in the formula IV undergoes reductive amination to obtain a compound as shown in the formula V; the compound as shown in the formula V and asymmetry acid undergo salifying to obtain a compound as shown in the formula VI; and the compound as shown in the formula VI reacts with 3-acetamido-phthalic anhydride to obtain Apremilast. By the method for synthesizing Apremilast, usage of an n-butyllithium hexane solution can be avoided. Production cost is reduced, and operation process is convenient. In addition, safety in the industrial production is raised to a great extent, and the preparation method is more suitable for industrial continuous production. According to the preparation method of 3-acetamido-phthalic anhydride, yield is raised to 81%. As the yield is high, the method provided by the invention is extremely suitable for industrial production of Apremilast.
Novel 3-Oxa-10-Aza-Phenanthrenes
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Page/Page column 16, (2010/11/28)
The compounds of formula I in which R1, R2 and R3 have the meanings as given in the description, are novel effective PDE4 inhibitors.